Darusentan (Lu-135252) is a selective endothelin receptor A ( ET-A ) receptor antagonist, which binds with a K i of 1.4 nM to the ET-A receptor and a K i of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K i of 13 nM.
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